PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 33609719-3 2021 This study investigated the in vitro efficacy of mefloquine in combination with colistin against 114 antibiotic-resistant Enterobacterales isolates including NDM-1, ESBL and mcr-1 containing strains from a broad range of origins. Mefloquine 49-59 Beta-lactamase Escherichia coli 158-163 3497888-1 1987 Effect of pyrimethamine, an antimalarial antifolate, and of mefloquine, chloroquine, and quinine, which belong to the quinoline group of antimalarials, on proliferation and interleukin 2 (IL-2) production of human lymphocytes was studied in vitro. Mefloquine 60-70 interleukin 2 Homo sapiens 173-186 33995308-4 2021 Mefloquine showed higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC50 = 1.28 muM, IC90 = 2.31 muM, and IC99 = 4.39 muM in VeroE6/TMPRSS2 cells. Mefloquine 0-10 transmembrane protease serine 2 Chlorocebus sabaeus 84-91 33995308-4 2021 Mefloquine showed higher anti-SARS-CoV-2 activity than Hydroxychloroquine in VeroE6/TMPRSS2 and Calu-3 cells, with IC50 = 1.28 muM, IC90 = 2.31 muM, and IC99 = 4.39 muM in VeroE6/TMPRSS2 cells. Mefloquine 0-10 transmembrane protease serine 2 Chlorocebus sabaeus 179-186 2858743-5 1985 The other trial showed that a single oral dose of 750 mg mefloquine and a single oral dose of MSP (750 mg mefloquine plus 3 tablets of "Fansidar", were equally effective in the treatment of falciparum malaria. Mefloquine 106-116 macrophage stimulating 1 Homo sapiens 94-97 2858743-9 1985 Mefloquine was well tolerated by patients with glucose-6-phosphate dehydrogenase deficiency or heterozygous haemoglobin E. Mefloquine 0-10 glucose-6-phosphate dehydrogenase Homo sapiens 47-80 6380785-1 1984 Camp and Smith strains of the human malaria parasite Plasmodium falciparum became resistant to mefloquine after continuous cultivation in the presence of the drug. Mefloquine 95-105 cathelicidin antimicrobial peptide Homo sapiens 0-4 6380785-5 1984 The mefloquine-resistant Camp strain remained sensitive to chloroquine and amodiaquine, and became slightly more resistant to quinine; there was increased sensitivity to pyrimethamine. Mefloquine 4-14 cathelicidin antimicrobial peptide Homo sapiens 25-29 33609719-3 2021 This study investigated the in vitro efficacy of mefloquine in combination with colistin against 114 antibiotic-resistant Enterobacterales isolates including NDM-1, ESBL and mcr-1 containing strains from a broad range of origins. Mefloquine 49-59 EsbL Escherichia coli 165-169 33609719-3 2021 This study investigated the in vitro efficacy of mefloquine in combination with colistin against 114 antibiotic-resistant Enterobacterales isolates including NDM-1, ESBL and mcr-1 containing strains from a broad range of origins. Mefloquine 49-59 melanocortin 1 receptor Mus musculus 174-179 33521428-3 2021 Mefloquine inhibits the binding of acyl-CoAs to acyl-CoA-binding proteins of Plasmodium falciparum (PfACBPs) and human (hACBP). Mefloquine 0-10 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 120-125 33521428-4 2021 In this study, we have used molecular dynamics simulation and other computational approaches to investigate the differences of stabilities of mefloquine-PfACBP749 and mefloquine-hACBP complexes. Mefloquine 167-177 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 178-183 33521428-6 2021 Although the essential tyrosine residues (tyrosine-30 and tyrosine-33 of PfACBP749 and tyrosine-29 and tyrosine-32 of hACBP) mediate the initial binding of mefloquine to the proteins by pi-stacking interactions, additional temporally longer interactions between mefloquine and aspartate-22 and methionine-25 of hACBP result in stronger binding of mefloquine to hACBP. Mefloquine 156-166 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 311-316 33521428-5 2021 The stability of mefloquine in the binding cavity of PfACBP749 is less than its stability in the binding pocket of hACBP. Mefloquine 17-27 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 115-120 33521428-8 2021 On the contrary, in the mefloquine-bound state, the stability of hACBP protein is less than the stability of PfACBP749. Mefloquine 24-34 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 65-70 33521428-6 2021 Although the essential tyrosine residues (tyrosine-30 and tyrosine-33 of PfACBP749 and tyrosine-29 and tyrosine-32 of hACBP) mediate the initial binding of mefloquine to the proteins by pi-stacking interactions, additional temporally longer interactions between mefloquine and aspartate-22 and methionine-25 of hACBP result in stronger binding of mefloquine to hACBP. Mefloquine 156-166 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 118-123 33521428-10 2021 This causes the induction of aggregation properties in the hACBP in the mefloquine-bound state. Mefloquine 72-82 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 59-64 33521428-6 2021 Although the essential tyrosine residues (tyrosine-30 and tyrosine-33 of PfACBP749 and tyrosine-29 and tyrosine-32 of hACBP) mediate the initial binding of mefloquine to the proteins by pi-stacking interactions, additional temporally longer interactions between mefloquine and aspartate-22 and methionine-25 of hACBP result in stronger binding of mefloquine to hACBP. Mefloquine 156-166 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 311-316 31987860-0 2020 Mefloquine binding to human acyl-CoA binding protein leads to redox stress mediated apoptotic death of human neuroblastoma cells. Mefloquine 0-10 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 28-52 33521428-11 2021 Taken together, we describe the mechanistic features that affect the differential dynamic stabilities of mefloquine-bound PfACBP749 and hACBP proteins. Mefloquine 105-115 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 136-141 32903470-5 2020 Thus, the present study provides new perspectives, (i) through the use of pharmaco-fUS, a new non-clinical imaging modality, to move forward drug discovery in AD and (ii) by the profiling of two drug treatments on brain dynamics, one used in AD: donepezil, and the other in development: donepezil combined with mefloquine (THN201) as a modulator of astrocyte network. Mefloquine 311-321 fused in sarcoma Mus musculus 83-86 32850358-9 2020 More importantly, patient-derived xenograft mouse models of ESCC with SDHC high expression were more sensitive to MQ treatment than low SDHC-expressing xenografts. Mefloquine 114-116 succinate dehydrogenase complex, subunit C, integral membrane protein Mus musculus 70-74 32850358-10 2020 Taken together, mefloquine inhibits ESCC tumor growth by inducing mitochondrial autophagy and SDHC plays a vital role in MQ-induced anti-tumor effect on ESCC. Mefloquine 121-123 succinate dehydrogenase complex, subunit C, integral membrane protein Mus musculus 94-98 33505244-10 2020 This Cx36 reduction persists after 1-h of recovery but recovered after 3-6 h. This acute downregulation of Cx36 by PTZ is likely maladaptive, as acute pharmacological blockade of Cx36 by mefloquine results in increased susceptibility to PTZ-induced neuronal hyperactivity. Mefloquine 187-197 gap junction protein delta 2 Homo sapiens 5-9 33505244-10 2020 This Cx36 reduction persists after 1-h of recovery but recovered after 3-6 h. This acute downregulation of Cx36 by PTZ is likely maladaptive, as acute pharmacological blockade of Cx36 by mefloquine results in increased susceptibility to PTZ-induced neuronal hyperactivity. Mefloquine 187-197 gap junction protein delta 2 Homo sapiens 107-111 33505244-10 2020 This Cx36 reduction persists after 1-h of recovery but recovered after 3-6 h. This acute downregulation of Cx36 by PTZ is likely maladaptive, as acute pharmacological blockade of Cx36 by mefloquine results in increased susceptibility to PTZ-induced neuronal hyperactivity. Mefloquine 187-197 gap junction protein delta 2 Homo sapiens 107-111 33067780-2 2020 Here, we established a mouse model of partial transection of the infraorbital nerve (pT-ION) and found that the Connexin 36 (Cx36) inhibitor mefloquine caused greater alleviation of pT-ION-induced cold allodynia compared to the reduction of mechanical allodynia. Mefloquine 141-151 gap junction protein, delta 2 Mus musculus 112-123 33067780-2 2020 Here, we established a mouse model of partial transection of the infraorbital nerve (pT-ION) and found that the Connexin 36 (Cx36) inhibitor mefloquine caused greater alleviation of pT-ION-induced cold allodynia compared to the reduction of mechanical allodynia. Mefloquine 141-151 gap junction protein, delta 2 Mus musculus 125-129 33067780-3 2020 Mefloquine reversed the pT-ION-induced upregulation of Cx36, glutamate receptor ionotropic kainate 2 (GluK2), transient receptor potential ankyrin 1 (TRPA1), and phosphorylated extracellular signal regulated kinase (p-ERK) in the trigeminal ganglion. Mefloquine 0-10 gap junction protein, delta 2 Mus musculus 55-59 33067780-3 2020 Mefloquine reversed the pT-ION-induced upregulation of Cx36, glutamate receptor ionotropic kainate 2 (GluK2), transient receptor potential ankyrin 1 (TRPA1), and phosphorylated extracellular signal regulated kinase (p-ERK) in the trigeminal ganglion. Mefloquine 0-10 glutamate receptor, ionotropic, kainate 2 (beta 2) Mus musculus 61-100 33067780-3 2020 Mefloquine reversed the pT-ION-induced upregulation of Cx36, glutamate receptor ionotropic kainate 2 (GluK2), transient receptor potential ankyrin 1 (TRPA1), and phosphorylated extracellular signal regulated kinase (p-ERK) in the trigeminal ganglion. Mefloquine 0-10 glutamate receptor, ionotropic, kainate 2 (beta 2) Mus musculus 102-107 33067780-3 2020 Mefloquine reversed the pT-ION-induced upregulation of Cx36, glutamate receptor ionotropic kainate 2 (GluK2), transient receptor potential ankyrin 1 (TRPA1), and phosphorylated extracellular signal regulated kinase (p-ERK) in the trigeminal ganglion. Mefloquine 0-10 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 110-148 33067780-3 2020 Mefloquine reversed the pT-ION-induced upregulation of Cx36, glutamate receptor ionotropic kainate 2 (GluK2), transient receptor potential ankyrin 1 (TRPA1), and phosphorylated extracellular signal regulated kinase (p-ERK) in the trigeminal ganglion. Mefloquine 0-10 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 150-155 33067780-3 2020 Mefloquine reversed the pT-ION-induced upregulation of Cx36, glutamate receptor ionotropic kainate 2 (GluK2), transient receptor potential ankyrin 1 (TRPA1), and phosphorylated extracellular signal regulated kinase (p-ERK) in the trigeminal ganglion. Mefloquine 0-10 mitogen-activated protein kinase 1 Mus musculus 218-221 32918165-1 2020 PURPOSE: To describe the development of progressive multifocal leukoencephalopathy (PML) in a patient with primary immune deficiency (PID) due to a NFKB1 (nuclear factor kB subunit 1) mutation, who was treated successfully with a combination of mirtazapine and mefloquine. Mefloquine 261-271 nuclear factor kappa B subunit 1 Homo sapiens 148-153 32918165-1 2020 PURPOSE: To describe the development of progressive multifocal leukoencephalopathy (PML) in a patient with primary immune deficiency (PID) due to a NFKB1 (nuclear factor kB subunit 1) mutation, who was treated successfully with a combination of mirtazapine and mefloquine. Mefloquine 261-271 nuclear factor kappa B subunit 1 Homo sapiens 155-182 31987860-6 2020 In this study, we show that mefloquine binds to and inactivates the human acyl-CoA binding protein (hACBP), potentially inducing redox stress in human neuroblastoma cells (IMR-32). Mefloquine 28-38 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 74-98 31987860-6 2020 In this study, we show that mefloquine binds to and inactivates the human acyl-CoA binding protein (hACBP), potentially inducing redox stress in human neuroblastoma cells (IMR-32). Mefloquine 28-38 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 100-105 31987860-7 2020 Mefloquine occupies the acyl-CoA binding pocket of hACBP by interacting with several of the critical acyl-CoA binding amino acids. Mefloquine 0-10 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 51-56 31987860-10 2020 Taken together, our study deciphers a mechanistic detail of how mefloquine leads to the death of human cells by perturbing the activity of hACBP and lipid homeostasis. Mefloquine 64-74 diazepam binding inhibitor, acyl-CoA binding protein Homo sapiens 139-144 31468346-6 2020 We found that these oscillations were totally abolished by bath application of a general blocker of gap junctions (carbenoxolone) or a specific blocker of electrical synapses (mefloquine), as determined by whole-cell recordings in both CA1 pyramidal cells and fast-spiking cells. Mefloquine 176-186 carbonic anhydrase 1 Homo sapiens 236-239 31691964-1 2020 The interaction between mefloquine (MEF), the antimalarial drug, and human serum albumin (HSA), the main carrier protein in blood circulation, was explored using fluorescence, absorption, and circular dichroism spectroscopic techniques. Mefloquine 24-34 albumin Homo sapiens 75-88 31276961-4 2019 This effect is selective as mefloquine is more effective in inducing apoptosis, inhibiting colony formation and self-renewal capacity of CD34+ cells derived from TKI-resistant BP-CML patients than normal cord blood (CB) CD34+ stem/progenitor cells. Mefloquine 28-38 CD34 molecule Homo sapiens 137-141 31276961-4 2019 This effect is selective as mefloquine is more effective in inducing apoptosis, inhibiting colony formation and self-renewal capacity of CD34+ cells derived from TKI-resistant BP-CML patients than normal cord blood (CB) CD34+ stem/progenitor cells. Mefloquine 28-38 CD34 molecule Homo sapiens 220-224 31276961-5 2019 Notably, the combination of mefloquine and TKIs at sublethal concentrations leads to synergistic effects in CML CD34+ cells, while sparing normal CB CD34+ cells. Mefloquine 28-38 CD34 molecule Homo sapiens 112-116 31276961-5 2019 Notably, the combination of mefloquine and TKIs at sublethal concentrations leads to synergistic effects in CML CD34+ cells, while sparing normal CB CD34+ cells. Mefloquine 28-38 CD34 molecule Homo sapiens 149-153 30882968-7 2019 We then showed that CD10 and CD11 are efficient chiral selectors for the capillary electrophoretic separation of the enantiomeric pharmaceuticals fluvastatin, mefloquine, carvedilol, and primaquine. Mefloquine 159-169 membrane metalloendopeptidase Homo sapiens 20-24 31120902-0 2019 The antimalarial drug mefloquine enhances TP53 premature termination codon readthrough by aminoglycoside G418. Mefloquine 22-32 tumor protein p53 Homo sapiens 42-46 31120902-7 2019 The two enantiomers composing pharmaceutical mefloquine potentiated readthrough to similar levels in HDQ-P1 cells and also in SW900, NCI-H1688 and HCC1937 cancer cells with different TP53 nonsense mutations. Mefloquine 45-55 tumor protein p53 Homo sapiens 183-187 31120902-8 2019 Exposure to G418 and mefloquine increased p53 phosphorylation at Ser15 and P21 transcript levels following DNA damage, indicating p53 produced via readthrough was functional. Mefloquine 21-31 tumor protein p53 Homo sapiens 42-45 31120902-8 2019 Exposure to G418 and mefloquine increased p53 phosphorylation at Ser15 and P21 transcript levels following DNA damage, indicating p53 produced via readthrough was functional. Mefloquine 21-31 H3 histone pseudogene 16 Homo sapiens 75-78 31120902-8 2019 Exposure to G418 and mefloquine increased p53 phosphorylation at Ser15 and P21 transcript levels following DNA damage, indicating p53 produced via readthrough was functional. Mefloquine 21-31 tumor protein p53 Homo sapiens 130-133 31110238-4 2019 The cells expressed Panx1 at the mRNA level, and released ATP in a manner that could be reduced by treatment with the Panx1 inhibitors carbenoxolone and mefloquine and the Panx1 substrate SR101. Mefloquine 153-163 pannexin 1 Homo sapiens 118-123 31110238-4 2019 The cells expressed Panx1 at the mRNA level, and released ATP in a manner that could be reduced by treatment with the Panx1 inhibitors carbenoxolone and mefloquine and the Panx1 substrate SR101. Mefloquine 153-163 pannexin 1 Homo sapiens 118-123 30765602-4 2019 In addition, we identified mefloquine hydrochloride, an antimalarial drug, as a novel RAB5/7 inhibitor and promising colorectal CSC-targeting drug. Mefloquine 27-51 RAB5A, member RAS oncogene family Homo sapiens 86-92 30765602-6 2019 In a patient-derived xenograft (PDX) model of colon cancer, treatment with mefloquine resulted in suppression of mitophagic PINK1/PARKIN and increased mitochondrial disorder and mitochondria-induced apoptosis without apparent side effects. Mefloquine 75-85 PTEN induced kinase 1 Homo sapiens 124-129 30765602-7 2019 These results suggest that the combination of mefloquine with chemotherapeutic agents in the PDX model potentially disrupts the hierarchy of colorectal cancer cells and identify endolysosomal RAB5/7 and LAMP1/2 as promising therapeutic targets in CSCs. Mefloquine 46-56 RAB5A, member RAS oncogene family Homo sapiens 192-198 30308940-2 2018 We show that nelfinavir and mefloquine synergize to selectively evoke a cytotoxic response in TSC2-deficient cell lines with mTORC1 hyperactivity. Mefloquine 28-38 CREB regulated transcription coactivator 1 Mus musculus 125-131 31112950-5 2019 Offspring were treated with the connexin 36 (Cx36) inhibitor mefloquine at postnatal day (P)1-P3 or at P40-P42. Mefloquine 61-71 gap junction protein, delta 2 Mus musculus 32-43 31112950-5 2019 Offspring were treated with the connexin 36 (Cx36) inhibitor mefloquine at postnatal day (P)1-P3 or at P40-P42. Mefloquine 61-71 gap junction protein, delta 2 Mus musculus 45-49 31112950-10 2019 Neonatal administration of the Cx36 inhibitor mefloquine could prevent these motor deficits. Mefloquine 46-56 gap junction protein, delta 2 Mus musculus 31-35 30308940-3 2018 We optimize the concentrations of nelfinavir and mefloquine to a clinically viable range that kill cells that lack TSC2, while wild-type cells tolerate treatment. Mefloquine 49-59 TSC complex subunit 2 Homo sapiens 115-119 30308940-8 2018 This work underpins a critical vulnerability with cancer cells with aberrant signaling through the TSC2-mTORC1 pathway that lack flexibility in homeostatic pathways, which could be exploited with combined nelfinavir and mefloquine treatment. Mefloquine 220-230 TSC complex subunit 2 Homo sapiens 99-103 30308940-8 2018 This work underpins a critical vulnerability with cancer cells with aberrant signaling through the TSC2-mTORC1 pathway that lack flexibility in homeostatic pathways, which could be exploited with combined nelfinavir and mefloquine treatment. Mefloquine 220-230 CREB regulated transcription coactivator 1 Mus musculus 104-110 29848662-9 2018 Pharmacological inhibition of pannexin-1 channels with probenecid or mefloquine-two medications currently used for treating gout and malaria, respectively-blocked ictal discharges in human cortical brain tissue slices. Mefloquine 69-79 pannexin 1 Homo sapiens 30-40 29221793-0 2018 Pannexin-1 channel dysfunction in the medial prefrontal cortex mediates depressive-like behaviors induced by chronic social defeat stress and administration of mefloquine in mice. Mefloquine 160-170 pannexin 1 Mus musculus 0-10 29221793-3 2018 Interestingly, MFQ is also known as a broad-spectrum pannexin-1 (Panx1) inhibitor. Mefloquine 15-18 pannexin 1 Mus musculus 53-63 29221793-3 2018 Interestingly, MFQ is also known as a broad-spectrum pannexin-1 (Panx1) inhibitor. Mefloquine 15-18 pannexin 1 Mus musculus 65-70 29221793-8 2018 Finally, systemic and intral-mPFC injection of MFQ both inhibited the activity of Panx1 and induced depressive-like and anxiety behaviors in mice with sub-threshold social defeat stress. Mefloquine 47-50 pannexin 1 Mus musculus 82-87 29221793-10 2018 In conclusion, our study demonstrates a role of the Panx1 channel in chronic stress and MFQ-induced depressive-like and anxiety behaviors, which may provide a novel molecular mechanism for psychiatric side effects of MFQ. Mefloquine 88-91 pannexin 1 Mus musculus 52-57 29208420-0 2018 The inhibitor of connexin Cx36 channels, mefloquine, inhibits voltage-dependent Ca2+ channels and insulin secretion. Mefloquine 41-51 gap junction protein, delta 2 Mus musculus 26-30 29208420-1 2018 The antimalarial agent, mefloquine, inhibits the function of connexin Cx36 gap junctions and hemichannels and has thus become a tool to investigate their physiological relevance in pancreatic islets. Mefloquine 24-34 gap junction protein, delta 2 Mus musculus 70-74 29879544-6 2018 Mefloquine administration did not change the levels of the circulating bone formation markers P1NP or alkaline phosphatase, whereas levels of the resorption marker CTX showed trends towards increase with mefloquine treatment. Mefloquine 204-214 V-set and immunoglobulin domain containing 2 Mus musculus 164-167 29879544-9 2018 Further, osteoclast numbers were higher on the endocortical bone surface and circulating CTX levels were increased, in mefloquine- compared to vehicle-treated young mice. Mefloquine 119-129 V-set and immunoglobulin domain containing 2 Mus musculus 89-92 29221793-10 2018 In conclusion, our study demonstrates a role of the Panx1 channel in chronic stress and MFQ-induced depressive-like and anxiety behaviors, which may provide a novel molecular mechanism for psychiatric side effects of MFQ. Mefloquine 217-220 pannexin 1 Mus musculus 52-57 29746991-9 2018 Pharmacological Cx36 blockade by intracisternal administration of mefloquine decreased significantly the mechanical allodynia observed in CCI-IoN-lesioned rats. Mefloquine 66-76 gap junction protein, delta 2 Rattus norvegicus 16-20 29453896-2 2018 In the present study, we found that the widely used antimalarial drug mefloquine was a NF-kappaB inhibitor that blocked the activation of IkappaBalpha kinase, leading to reduction of IkappaBalpha degradation, decrease of p65 phosphorylation, and suppressed expression of NF-kappaB target genes in CRC cells. Mefloquine 70-80 v-rel reticuloendotheliosis viral oncogene homolog A (avian) Mus musculus 221-224 29578061-0 2018 Mefloquine targets beta-catenin pathway and thus can play a role in the treatment of liver cancer. Mefloquine 0-10 catenin beta 1 Homo sapiens 19-31 29578061-4 2018 Mefloquine treatment of CD133 + HepG2 cells inhibited the proliferation selectively in concentration based manner. Mefloquine 0-10 prominin 1 Homo sapiens 24-29 29578061-5 2018 The rate of proliferation was inhibited to 82 and 12% in parental and CD133 + sphere forming cells, respectively on treatment with 10 muM concentration of mefloquine. Mefloquine 155-165 prominin 1 Homo sapiens 70-75 29578061-7 2018 Treatment of the liver cancer stem cells with mefloquine markedly decreased the potential to undergo self-renewal at 10 muM concentration after 48 h. The results from western blot analysis showed significantly higher expression of cancer stem cell molecules beta-catenin and cyclin D1 in LCSCs. Mefloquine 46-56 catenin beta 1 Homo sapiens 258-270 29578061-7 2018 Treatment of the liver cancer stem cells with mefloquine markedly decreased the potential to undergo self-renewal at 10 muM concentration after 48 h. The results from western blot analysis showed significantly higher expression of cancer stem cell molecules beta-catenin and cyclin D1 in LCSCs. Mefloquine 46-56 cyclin D1 Homo sapiens 275-284 29578061-8 2018 Treatment of the LCSCs with various concentrations of mefloquine reduced the expression levels of beta-catenin and cyclin D1. Mefloquine 54-64 catenin beta 1 Homo sapiens 98-110 29578061-8 2018 Treatment of the LCSCs with various concentrations of mefloquine reduced the expression levels of beta-catenin and cyclin D1. Mefloquine 54-64 cyclin D1 Homo sapiens 115-124 29578061-12 2018 Thus, mefloquine treatment inhibits self-renewal and proliferation potential of cells through targeting beta-catenin pathway. Mefloquine 6-16 catenin beta 1 Homo sapiens 104-116 29453896-0 2018 Antimalarial drug mefloquine inhibits nuclear factor kappa B signaling and induces apoptosis in colorectal cancer cells. Mefloquine 18-28 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 38-60 29453896-2 2018 In the present study, we found that the widely used antimalarial drug mefloquine was a NF-kappaB inhibitor that blocked the activation of IkappaBalpha kinase, leading to reduction of IkappaBalpha degradation, decrease of p65 phosphorylation, and suppressed expression of NF-kappaB target genes in CRC cells. Mefloquine 70-80 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 87-96 29453896-2 2018 In the present study, we found that the widely used antimalarial drug mefloquine was a NF-kappaB inhibitor that blocked the activation of IkappaBalpha kinase, leading to reduction of IkappaBalpha degradation, decrease of p65 phosphorylation, and suppressed expression of NF-kappaB target genes in CRC cells. Mefloquine 70-80 nuclear factor of kappa light polypeptide gene enhancer in B cells inhibitor, alpha Mus musculus 138-150 29453896-2 2018 In the present study, we found that the widely used antimalarial drug mefloquine was a NF-kappaB inhibitor that blocked the activation of IkappaBalpha kinase, leading to reduction of IkappaBalpha degradation, decrease of p65 phosphorylation, and suppressed expression of NF-kappaB target genes in CRC cells. Mefloquine 70-80 nuclear factor of kappa light polypeptide gene enhancer in B cells inhibitor, alpha Mus musculus 183-195 29744272-0 2018 Antidiabetic activity of mefloquine via GLP-1 receptor modulation against STZ-NA-induced diabetes in albino wistar rats. Mefloquine 25-35 glucagon-like peptide 1 receptor Rattus norvegicus 40-54 29453896-2 2018 In the present study, we found that the widely used antimalarial drug mefloquine was a NF-kappaB inhibitor that blocked the activation of IkappaBalpha kinase, leading to reduction of IkappaBalpha degradation, decrease of p65 phosphorylation, and suppressed expression of NF-kappaB target genes in CRC cells. Mefloquine 70-80 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 271-280 29453896-3 2018 We also found that mefloquine induced growth arrest and apoptosis of CRC cells harboring phosphorylated p65 in culture and in mice. Mefloquine 19-29 v-rel reticuloendotheliosis viral oncogene homolog A (avian) Mus musculus 104-107 29453896-5 2018 These results showed that mefloquine could exert antitumor action through inhibiting the NF-kappaB signaling pathway, and indicated that the antimalarial drug might be repurposed for anti-CRC therapy in the clinic as a single agent or in combination with other anticancer drugs. Mefloquine 26-36 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 89-98 28134928-10 2017 Treatment with a Panx1-blocking peptide (10panx) or the clinically used broad-spectrum Panx1 blockers, mefloquine or probenecid, suppressed ATP release and reduced withdrawal severity. Mefloquine 103-113 pannexin 1 Homo sapiens 87-92 28475285-12 2017 Furthermore, 18beta-glycyrrhetinic acids and mefloquine, which are gap junction inhibitors, attenuated senktide-induced Ca2+ oscillations in Kiss1-GFP cells. Mefloquine 45-55 KiSS-1 metastasis-suppressor Mus musculus 141-146 28879898-0 2017 Progressive multifocal leukoencephalopathy in a 44-year old male with idiopathic CD4+ T-lymphocytopenia treated with mirtazapine and mefloquine. Mefloquine 133-143 CD4 molecule Homo sapiens 81-84 27941941-3 2016 Using primary cultures, we found that both mefloquine and amitriptyline inhibited Cx43-containing gap junctions, and that the drug combination acted synergically. Mefloquine 43-53 gap junction protein, alpha 1 Rattus norvegicus 82-86 28068604-5 2017 We found that quinoline derivatives 3a and 4 were the most potent compounds within this series, both with mean EC50 values of 0.8 muM, which represents a potency 5 times that of mefloquine. Mefloquine 178-188 latexin Homo sapiens 130-133 28057491-0 2017 Mefloquine inhibits voltage dependent Nav1.4 channel by overlapping the local anaesthetic binding site. Mefloquine 0-10 sodium voltage-gated channel alpha subunit 4 Homo sapiens 38-44 28057491-4 2017 We found that mefloquine: i) inhibited Nav1.4 currents (IC50 =60muM), ii) significantly delayed fast inactivation but did not affect recovery from inactivation, iii) markedly the shifted steady-state inactivation curve to more hyperpolarized potentials. Mefloquine 14-24 sodium voltage-gated channel alpha subunit 4 Homo sapiens 39-45 28057491-5 2017 The presence of the beta1 subunit significantly reduced mefloquine potency, but the drug induced a significant frequency-independent rundown upon repetitive depolarisations. Mefloquine 56-66 potassium calcium-activated channel subfamily M regulatory beta subunit 1 Homo sapiens 20-25 28057491-7 2017 This is supported by the fact that mefloquine potency significantly decreased on mutant Nav1.4 channel F1579A and significantly increased on K1237S channels. Mefloquine 35-45 sodium voltage-gated channel alpha subunit 4 Homo sapiens 88-94 27831748-0 2017 Therapeutic effects of antibiotic drug mefloquine against cervical cancer through impairing mitochondrial function and inhibiting mTOR pathway. Mefloquine 39-49 mechanistic target of rapamycin kinase Homo sapiens 130-134 27831748-6 2017 We further show that mefloquine suppresses activation of mTOR signaling pathway in HeLa cells. Mefloquine 21-31 mechanistic target of rapamycin kinase Homo sapiens 57-61 27831748-8 2017 Inhibition of mTOR signaling pathway by mefloquine was also reversed in HeLa rho0 cells, suggesting deactivation of mTOR pathway as a consequence of mitochondria function disruption. Mefloquine 40-50 mechanistic target of rapamycin kinase Homo sapiens 14-18 27831748-8 2017 Inhibition of mTOR signaling pathway by mefloquine was also reversed in HeLa rho0 cells, suggesting deactivation of mTOR pathway as a consequence of mitochondria function disruption. Mefloquine 40-50 mechanistic target of rapamycin kinase Homo sapiens 116-120 26422780-0 2015 A Concise and Highly Enantioselective Total Synthesis of (+)-anti- and (-)-syn-Mefloquine Hydrochloride: Definitive Absolute Stereochemical Assignment of the Mefloquines. Mefloquine 158-169 synemin Homo sapiens 75-78 27793909-3 2016 MATERIALS AND METHODS: The anti-malarial drugs chloroquine (CHL), mefloquine (MEF) and primaquine (PRI) have been shown to increase sensitization in drug-resistant KBV20C cells via P-gp inhibition. Mefloquine 66-76 ATP binding cassette subfamily B member 1 Homo sapiens 181-185 26824480-4 2016 Those infected mice treated with both silymarin and mefloquine showed a significant decrease (P < 0.001) in worm burden, immunoglobulins (IgG and IgM), liver function enzymes and granuloma diameter, with complete eradication of immature and mature eggs. Mefloquine 52-62 immunoglobulin heavy constant mu Mus musculus 150-153 27657347-5 2016 X-ray crystallographic analysis of derivatives of (+)-anti- and (-)-syn-mefloquine is used to lay to rest a 40 year argument regarding the absolute stereochemistry of the mefloquines. Mefloquine 171-182 synemin Homo sapiens 68-71 27045516-10 2016 Mefloquine was shown to be a P-gp inhibitor affecting our P-gp substrate, Rhodamine 123, although none of the other drugs impacted upon rhodamine123 transport rates. Mefloquine 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 29-33 27045516-10 2016 Mefloquine was shown to be a P-gp inhibitor affecting our P-gp substrate, Rhodamine 123, although none of the other drugs impacted upon rhodamine123 transport rates. Mefloquine 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 27045516-11 2016 In conclusion, mefloquine is a P-gp inhibitor and methylene blue is a partial substrate; methylene blue may have increased absorption if co-administered with such P-gp inhibitors. Mefloquine 15-25 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 27045516-11 2016 In conclusion, mefloquine is a P-gp inhibitor and methylene blue is a partial substrate; methylene blue may have increased absorption if co-administered with such P-gp inhibitors. Mefloquine 15-25 ATP binding cassette subfamily B member 1 Homo sapiens 163-167 27045516-12 2016 An upregulation of P-gp was observed when artemisone and dihydroartemisinin were co-incubated with mefloquine and amodiaquine. Mefloquine 99-109 ATP binding cassette subfamily B member 1 Homo sapiens 19-23 26780727-0 2016 Mefloquine effectively targets gastric cancer cells through phosphatase-dependent inhibition of PI3K/Akt/mTOR signaling pathway. Mefloquine 0-10 AKT serine/threonine kinase 1 Homo sapiens 101-104 26780727-0 2016 Mefloquine effectively targets gastric cancer cells through phosphatase-dependent inhibition of PI3K/Akt/mTOR signaling pathway. Mefloquine 0-10 mechanistic target of rapamycin kinase Homo sapiens 105-109 26780727-6 2016 In addition, mefloquine potently decreased phosphorylation of PI3K, Akt, mTOR and rS6. Mefloquine 13-23 AKT serine/threonine kinase 1 Homo sapiens 68-71 26780727-6 2016 In addition, mefloquine potently decreased phosphorylation of PI3K, Akt, mTOR and rS6. Mefloquine 13-23 mechanistic target of rapamycin kinase Homo sapiens 73-77 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 67-77 AKT serine/threonine kinase 1 Homo sapiens 40-43 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 67-77 mechanistic target of rapamycin kinase Homo sapiens 101-105 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 67-77 AKT serine/threonine kinase 1 Homo sapiens 239-242 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 67-77 mechanistic target of rapamycin kinase Homo sapiens 243-247 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 178-188 AKT serine/threonine kinase 1 Homo sapiens 40-43 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 178-188 mechanistic target of rapamycin kinase Homo sapiens 101-105 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 178-188 AKT serine/threonine kinase 1 Homo sapiens 239-242 26780727-7 2016 Overexpression of constitutively active Akt significantly restored mefloquine-mediated inhibition of mTOR phosphorylation and growth, and induction of apoptosis, suggesting that mefloquine acts on gastric cancer cells via suppressing PI3K/Akt/mTOR pathway. Mefloquine 178-188 mechanistic target of rapamycin kinase Homo sapiens 243-247 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 21-31 AKT serine/threonine kinase 1 Homo sapiens 55-58 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 21-31 mechanistic target of rapamycin kinase Homo sapiens 59-63 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 21-31 AKT serine/threonine kinase 1 Homo sapiens 192-195 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 21-31 mechanistic target of rapamycin kinase Homo sapiens 196-200 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 158-168 AKT serine/threonine kinase 1 Homo sapiens 55-58 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 158-168 mechanistic target of rapamycin kinase Homo sapiens 59-63 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 158-168 AKT serine/threonine kinase 1 Homo sapiens 192-195 26780727-8 2016 We further show that mefloquine-mediated inhibition of Akt/mTOR singaling is phosphatase-dependent as pretreatment with calyculin A does-dependently reversed mefloquine-mediated inhibition of Akt/mTOR phosphorylation. Mefloquine 158-168 mechanistic target of rapamycin kinase Homo sapiens 196-200 30404280-15 2016 For example, the effect of mefloquine, a medication used to treat malaria, on the electrical activity of neuronal cells was determined in this study using a GC3 system. Mefloquine 27-37 ankyrin repeat domain 36 Mus musculus 157-160 26422780-6 2015 These are the first X-ray structures for mefloquine derivatives that were obtained by coupling to a known chiral, nonracemic compound, and provide definitive confirmation of the absolute stereochemistry of (+)-anti- as well as (-)-syn-mefloquine. Mefloquine 41-51 synemin Homo sapiens 231-234 26722448-8 2015 On the other hand, mefloquine treatment promoted the expression of p21WAF1/CIP1 and p53 at 40 muM concentration after 48 h. Therefore, mefloquine inhibits proliferation and induces cell cycle arrest in chondrocytes. Mefloquine 19-29 cyclin dependent kinase inhibitor 1A Homo sapiens 75-79 27621501-0 2015 FDA Advise-ERR: Mefloquine-Not the Same as Malarone; Zoster Vaccine Is Not for the Immunosuppressed; TXA Mistaken as Tenecteplase; Guidelines for Adult IV Push Medications. Mefloquine 16-26 solute carrier family 7 member 1 Homo sapiens 11-14 26216464-0 2015 Modulation of the transient outward current (Ito) in rat cardiac myocytes and human Kv4.3 channels by mefloquine. Mefloquine 102-112 potassium voltage-gated channel subfamily D member 3 Homo sapiens 84-89 26216464-1 2015 The antimalarial drug mefloquine, is known to be a potassium channel blocker, although its mechanism of action has not being elucidated and its effects on the transient outward current (Ito) and the molecular correlate, the Kv4.3 channel has not being studied. Mefloquine 22-32 potassium voltage-gated channel subfamily D member 3 Rattus norvegicus 224-229 26216464-2 2015 Here, we describe the mefloquine-induced inhibition of the rat ventricular Ito and of CHO cells co-transfected with human Kv4.3 and its accessory subunit hKChIP2C by whole-cell voltage-clamp. Mefloquine 22-32 potassium voltage-gated channel subfamily D member 3 Homo sapiens 122-127 26216464-3 2015 Mefloquine inhibited rat Ito and hKv4.3+KChIP2C currents in a concentration-dependent manner with a limited voltage dependence and similar potencies (IC50=8.9muM and 10.5muM for cardiac myocytes and Kv4.3 channels, respectively). Mefloquine 0-10 potassium voltage-gated channel subfamily D member 3 Homo sapiens 33-39 26216464-3 2015 Mefloquine inhibited rat Ito and hKv4.3+KChIP2C currents in a concentration-dependent manner with a limited voltage dependence and similar potencies (IC50=8.9muM and 10.5muM for cardiac myocytes and Kv4.3 channels, respectively). Mefloquine 0-10 potassium voltage-gated channel subfamily D member 3 Rattus norvegicus 34-39 26216464-4 2015 In addition, mefloquine did not affect the activation of either current but significantly modified the hKv4.3 steady-state inactivation and recovery from inactivation. Mefloquine 13-23 potassium voltage-gated channel subfamily D member 3 Homo sapiens 103-109 26722448-8 2015 On the other hand, mefloquine treatment promoted the expression of p21WAF1/CIP1 and p53 at 40 muM concentration after 48 h. Therefore, mefloquine inhibits proliferation and induces cell cycle arrest in chondrocytes. Mefloquine 19-29 tumor protein p53 Homo sapiens 84-87 26722448-8 2015 On the other hand, mefloquine treatment promoted the expression of p21WAF1/CIP1 and p53 at 40 muM concentration after 48 h. Therefore, mefloquine inhibits proliferation and induces cell cycle arrest in chondrocytes. Mefloquine 135-145 cyclin dependent kinase inhibitor 1A Homo sapiens 75-79 26722448-8 2015 On the other hand, mefloquine treatment promoted the expression of p21WAF1/CIP1 and p53 at 40 muM concentration after 48 h. Therefore, mefloquine inhibits proliferation and induces cell cycle arrest in chondrocytes. Mefloquine 135-145 tumor protein p53 Homo sapiens 84-87 25947940-3 2015 We show here that Panx1 forms ATP release channels in human platelets and that inhibiting Panx1 channel function with probenecid, mefloquine or specific (10)Panx1 peptides reduces collagen-induced platelet aggregation but not the response induced by arachidonic acid or ADP. Mefloquine 130-140 pannexin 1 Homo sapiens 90-95 25491783-0 2015 Effect of Mefloquine, a Gap Junction Blocker, on Circadian Period2 Gene Oscillation in the Mouse Suprachiasmatic Nucleus Ex Vivo. Mefloquine 10-20 period circadian clock 2 Mus musculus 59-66 25491783-4 2015 METHODS: We examined the effect of mefloquine, a neuronal gap junction blocker, on circadian Period 2 (Per2) gene oscillation in SCN slice cultures prepared from Per2::luciferase (PER2::LUC) knock-in mice using a real-time bioluminescence measurement system. Mefloquine 35-45 period circadian clock 2 Mus musculus 93-101 25491783-4 2015 METHODS: We examined the effect of mefloquine, a neuronal gap junction blocker, on circadian Period 2 (Per2) gene oscillation in SCN slice cultures prepared from Per2::luciferase (PER2::LUC) knock-in mice using a real-time bioluminescence measurement system. Mefloquine 35-45 period circadian clock 2 Mus musculus 103-107 25491783-5 2015 RESULTS: Administration of mefloquine causes instability in the pulse period and a slight reduction of amplitude in cyclic PER2::LUC expression. Mefloquine 27-37 period circadian clock 2 Mus musculus 123-127 25947940-3 2015 We show here that Panx1 forms ATP release channels in human platelets and that inhibiting Panx1 channel function with probenecid, mefloquine or specific (10)Panx1 peptides reduces collagen-induced platelet aggregation but not the response induced by arachidonic acid or ADP. Mefloquine 130-140 pannexin 1 Homo sapiens 90-95 25796110-12 2015 IPC-induced neuroprotective effects were significantly abolished by pretreatment of mefloquine (15.0 mg/kg orally; 30.0 mg/kg orally), blocker of Panx1/P2X7 purinoceptor. Mefloquine 84-94 pannexin 1 Mus musculus 146-151 25796110-12 2015 IPC-induced neuroprotective effects were significantly abolished by pretreatment of mefloquine (15.0 mg/kg orally; 30.0 mg/kg orally), blocker of Panx1/P2X7 purinoceptor. Mefloquine 84-94 purinergic receptor P2X, ligand-gated ion channel, 7 Mus musculus 152-169 24284282-0 2013 Co-treatment with the anti-malarial drugs mefloquine and primaquine highly sensitizes drug-resistant cancer cells by increasing P-gp inhibition. Mefloquine 42-52 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 25229253-0 2015 Aberrant connexin26 hemichannels underlying keratitis-ichthyosis-deafness syndrome are potently inhibited by mefloquine. Mefloquine 109-119 gap junction protein beta 2 Homo sapiens 9-19 25229253-8 2015 Furthermore, we used freshly isolated transgenic keratinocytes to show that micromolar concentrations of MFQ attenuated increased macroscopic membrane currents in primary mouse keratinocytes expressing human Cx26-G45E, a mutation that causes a lethal form of KID syndrome. Mefloquine 105-108 gap junction protein beta 2 Homo sapiens 208-212 25637780-2 2015 This concept mainly relied on using mefloquine 10-20muM as a putative selective Px1 channel-blocking agent to completely inhibit the contraction to phenylephrine, but not K(+) 40mM. Mefloquine 36-46 pannexin 1 Mus musculus 80-83 25637780-4 2015 The purpose of the present study was to explore the specificity of mefloquine for Px1 channels and the role of these channels in small artery contraction. Mefloquine 67-77 pannexin 1 Mus musculus 82-85 25637780-6 2015 Mefloquine had a wide range of inhibitory actions at 10-20muM, some 200-fold above the concentrations previously shown to inhibit expressed Px1 channel activity. Mefloquine 0-10 pannexin 1 Mus musculus 140-143 25637780-7 2015 Mefloquine 3-10muM inhibited phenylephrine, U46619, vasopressin, endothelin-1, sympathetic nerve stimulation and K(+) 40mM-mediated contractions in rat and mouse small mesenteric, and mouse thoracodorsal, arteries. Mefloquine 0-10 arginine vasopressin Rattus norvegicus 52-63 25637780-7 2015 Mefloquine 3-10muM inhibited phenylephrine, U46619, vasopressin, endothelin-1, sympathetic nerve stimulation and K(+) 40mM-mediated contractions in rat and mouse small mesenteric, and mouse thoracodorsal, arteries. Mefloquine 0-10 endothelin 1 Rattus norvegicus 65-77 25313206-0 2015 Carboxymefloquine, the major metabolite of the antimalarial drug mefloquine, induces drug-metabolizing enzyme and transporter expression by activation of pregnane X receptor. Mefloquine 7-17 nuclear receptor subfamily 1 group I member 2 Homo sapiens 154-173 25313206-5 2015 We screened 16 clinically used antimalarial drugs and six major drug metabolites for binding to PXR using the two-hybrid PXR ligand binding domain assembly assay; this identified carboxymefloquine, the major and pharmacologically inactive metabolite of the antimalarial drug mefloquine, as a potential PXR ligand. Mefloquine 186-196 nuclear receptor subfamily 1 group I member 2 Homo sapiens 96-99 25313206-5 2015 We screened 16 clinically used antimalarial drugs and six major drug metabolites for binding to PXR using the two-hybrid PXR ligand binding domain assembly assay; this identified carboxymefloquine, the major and pharmacologically inactive metabolite of the antimalarial drug mefloquine, as a potential PXR ligand. Mefloquine 186-196 nuclear receptor subfamily 1 group I member 2 Homo sapiens 121-124 25313206-5 2015 We screened 16 clinically used antimalarial drugs and six major drug metabolites for binding to PXR using the two-hybrid PXR ligand binding domain assembly assay; this identified carboxymefloquine, the major and pharmacologically inactive metabolite of the antimalarial drug mefloquine, as a potential PXR ligand. Mefloquine 186-196 nuclear receptor subfamily 1 group I member 2 Homo sapiens 121-124 24874696-9 2014 More large studies in other ethnic groups including polymorphism studies for the gene encoding P-glycoprotein (ABCB1/MDR1) and taking into account various underlying conditions with secondary immunosuppression should be carried out to investigate whether mefloquine is effective for treating PML. Mefloquine 255-265 ATP binding cassette subfamily B member 1 Homo sapiens 95-109 24735890-6 2014 Cx36 hemichannels expressed in oocytes opened upon depolarization of membrane potential, and their activation was inhibited by mefloquine and glucose (IC50 ~8 mM). Mefloquine 127-137 gap junction protein, delta 2 Mus musculus 0-4 24735890-9 2014 Mefloquine targeting of Cx36 on both gap junctions and hemichannels also suppresses glucose-stimulated secretion. Mefloquine 0-10 gap junction protein, delta 2 Mus musculus 24-28 23499662-4 2013 Most gap junction blockers also attenuate the function of Panx1, including carbenoxolone, mefloquine and flufenamic acid. Mefloquine 90-100 pannexin 1 Homo sapiens 58-63 26159705-5 2015 RESULTS: A 48 h treatment of human erythrocytes with mefloquine significantly increased the percentage of annexin-V-binding cells (>=5 mug/ml), significantly decreased forward scatter (>=5 mug/ml), significantly increased ROS abundance (5 mug/ml), significantly increased [Ca2+]i (7.5 mug/ml) and significantly increased ceramide abundance (10 mug/ml). Mefloquine 53-63 annexin A5 Homo sapiens 106-115 26159705-7 2015 Even in the absence of extracellular Ca2+, mefloquine significantly increased annexin-V-binding. Mefloquine 43-53 annexin A5 Homo sapiens 78-87 25170954-4 2014 ATP release from isolated rat bladders induced by distention was reduced by the Panx1 channel blocker mefloquine (MFQ) and was blunted in mice lacking Panx1 or P2X7R expression. Mefloquine 102-112 Pannexin 1 Rattus norvegicus 80-85 25170954-4 2014 ATP release from isolated rat bladders induced by distention was reduced by the Panx1 channel blocker mefloquine (MFQ) and was blunted in mice lacking Panx1 or P2X7R expression. Mefloquine 114-117 Pannexin 1 Rattus norvegicus 80-85 25170954-5 2014 Hypoosmotic shock induced YoPro dye uptake was inhibited by MFQ and the P2X7R blocker A438079 in TRT-HU1 cells, and was also blunted in primary urothelial cells derived from mice lacking Panx1 or P2X7R expression. Mefloquine 60-63 pannexin 1 Mus musculus 187-192 25170954-5 2014 Hypoosmotic shock induced YoPro dye uptake was inhibited by MFQ and the P2X7R blocker A438079 in TRT-HU1 cells, and was also blunted in primary urothelial cells derived from mice lacking Panx1 or P2X7R expression. Mefloquine 60-63 purinergic receptor P2X, ligand-gated ion channel, 7 Mus musculus 196-201 24488404-4 2014 RESULTS: Hallucinogens and mefloquine bound stereoselectively and with relatively high affinity (K i = 0.71-341 nM) to serotonin (5-HT) 2A but not 5-HT1A or 5-HT2C receptors. Mefloquine 27-37 5-hydroxytryptamine receptor 2C Homo sapiens 157-163 24488404-5 2014 Mefloquine but not chloroquine was a partial 5-HT2A agonist and a full 5-HT2C agonist, stimulating inositol phosphate accumulation, with similar potency and efficacy as the hallucinogen dimethyltryptamine (DMT). Mefloquine 0-10 5-hydroxytryptamine receptor 2A Homo sapiens 45-51 24488404-5 2014 Mefloquine but not chloroquine was a partial 5-HT2A agonist and a full 5-HT2C agonist, stimulating inositol phosphate accumulation, with similar potency and efficacy as the hallucinogen dimethyltryptamine (DMT). Mefloquine 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 71-77 24735890-3 2014 Cx36(+/+) islets lost ATP after depolarization with 70 mM KCl at 5 mM glucose; ATP loss was prevented by 8 and 20 mM glucose or 50 muM mefloquine (connexin inhibitor). Mefloquine 135-145 gap junction protein, delta 2 Mus musculus 0-4 24223197-0 2013 Addition of exogenous NAD+ prevents mefloquine-induced neuroaxonal and hair cell degeneration through reduction of caspase-3-mediated apoptosis in cochlear organotypic cultures. Mefloquine 36-46 caspase 3 Rattus norvegicus 115-124 23885286-6 2013 Additionally, pharmacologic inhibition of Panx1 channels with mefloquine (MFQ) reduced severity of acute and chronic EAE when administered before or after onset of clinical signs. Mefloquine 62-72 pannexin 1 Mus musculus 42-47 23885286-6 2013 Additionally, pharmacologic inhibition of Panx1 channels with mefloquine (MFQ) reduced severity of acute and chronic EAE when administered before or after onset of clinical signs. Mefloquine 74-77 pannexin 1 Mus musculus 42-47 23759954-9 2013 The MQ treatment mediated G1 cell cycle arrest and cyclin D1 accumulation through p21 upregulation in the PC3 cells. Mefloquine 4-6 cyclin D1 Mus musculus 51-60 23759954-9 2013 The MQ treatment mediated G1 cell cycle arrest and cyclin D1 accumulation through p21 upregulation in the PC3 cells. Mefloquine 4-6 cyclin-dependent kinase inhibitor 1A (P21) Mus musculus 82-85 23760395-11 2013 Moreover, we observed that MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells. Mefloquine 27-29 mitogen-activated protein kinase 1 Homo sapiens 145-148 23760395-0 2013 Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling. Mefloquine 0-10 AKT serine/threonine kinase 1 Homo sapiens 94-97 23760395-0 2013 Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling. Mefloquine 0-10 mitogen-activated protein kinase 1 Homo sapiens 99-102 23760395-11 2013 Moreover, we observed that MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells. Mefloquine 27-29 mitogen-activated protein kinase 8 Homo sapiens 151-174 23760395-11 2013 Moreover, we observed that MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells. Mefloquine 27-29 mitogen-activated protein kinase 8 Homo sapiens 176-179 23760395-0 2013 Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling. Mefloquine 0-10 mitogen-activated protein kinase 8 Homo sapiens 104-107 23760395-11 2013 Moreover, we observed that MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells. Mefloquine 27-29 AKT serine/threonine kinase 1 Homo sapiens 72-75 23760395-11 2013 Moreover, we observed that MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells. Mefloquine 27-29 mitogen-activated protein kinase 1 Homo sapiens 106-143 21638336-5 2011 Cx36 KO mice, and WT mice treated with the Cx36 antagonist mefloquine (MFQ), consumed significantly less ethanol than their WT controls in the drink-in-the-dark procedure. Mefloquine 59-69 gap junction protein, delta 2 Mus musculus 43-47 23827947-8 2013 Mefloquine (Panx1 blocker) reduced these IL-1beta responses. Mefloquine 0-10 pannexin 1 Mus musculus 12-17 23827947-8 2013 Mefloquine (Panx1 blocker) reduced these IL-1beta responses. Mefloquine 0-10 interleukin 1 beta Mus musculus 41-49 22846785-9 2012 We show that the protection achieved following sporozoite inoculation with concurrent mefloquine treatment is almost entirely dependent of CD8(+) T-cells. Mefloquine 86-96 CD8a molecule Homo sapiens 139-142 22465322-5 2012 Moreover, Mefloquine-induced autophagy was efficiently suppressed by an autophagy inhibitor and by down regulation of ATG6. Mefloquine 10-20 beclin 1 Homo sapiens 118-122 21241737-6 2011 Furthermore, we have utilized a system biology-centered approach and have constructed a pathway model of cellular responses to mefloquine, identifying non-receptor tyrosine kinase 2 (Pyk2) as a critical target in mediating mefloquine neurotoxicity. Mefloquine 127-137 protein tyrosine kinase 2 beta Rattus norvegicus 183-187 21685263-7 2011 Antagonists of both pannexin-1 (carbenoxolone and mefloquine) and P2X(7) receptors (brilliant blue G and A438079) blocked ATP pre- and postconditioning, indicating that ATP protection was elicited via the opening of a pannexin-1/P2X(7) channel. Mefloquine 50-60 Pannexin 1 Rattus norvegicus 20-30 21218452-0 2011 Mefloquine effects on ventral tegmental area dopamine and GABA neuron inhibition: a physiologic role for connexin-36 GAP junctions. Mefloquine 0-10 gap junction protein, delta 2 Mus musculus 105-116 21218452-4 2011 In brain slices from adolescent wild-type (WT) mice the Cx36-selective GJ blocker mefloquine (MFQ, 25 muM) increased VTA DA neuron sIPSC frequency sixfold, and mIPSC frequency threefold. Mefloquine 82-92 gap junction protein, delta 2 Mus musculus 56-60 21218452-4 2011 In brain slices from adolescent wild-type (WT) mice the Cx36-selective GJ blocker mefloquine (MFQ, 25 muM) increased VTA DA neuron sIPSC frequency sixfold, and mIPSC frequency threefold. Mefloquine 94-97 gap junction protein, delta 2 Mus musculus 56-60 21218452-8 2011 We also examined MFQ effects on VTA DA neuron firing rate and current-evoked spiking in WT and Cx36 KO mice, and found that MFQ decreased WT DA neuron firing rate and current-evoked spiking, but did not alter these measures in Cx36 KO mice. Mefloquine 124-127 gap junction protein, delta 2 Mus musculus 95-99 21218452-8 2011 We also examined MFQ effects on VTA DA neuron firing rate and current-evoked spiking in WT and Cx36 KO mice, and found that MFQ decreased WT DA neuron firing rate and current-evoked spiking, but did not alter these measures in Cx36 KO mice. Mefloquine 124-127 gap junction protein, delta 2 Mus musculus 227-231 23318648-0 2013 MDR1-associated resistance to artesunate+mefloquine does not impair blood-stage parasite fitness in a rodent malaria model. Mefloquine 41-51 malic enzyme complex, mitochondrial Mus musculus 0-4 22986170-10 2012 Finally, to elucidate whether the gap junction blocker mefloquine (MFQ) previously shown to dampen ACx SOs in slices affected GABAergic transmission, MFQ was acutely applied in P3-5 slices while spontaneous inhibitory postsynaptic currents (sIPSCs) were recorded. Mefloquine 55-65 cyclin dependent kinase 5 regulatory subunit 1 Homo sapiens 177-181 22986170-10 2012 Finally, to elucidate whether the gap junction blocker mefloquine (MFQ) previously shown to dampen ACx SOs in slices affected GABAergic transmission, MFQ was acutely applied in P3-5 slices while spontaneous inhibitory postsynaptic currents (sIPSCs) were recorded. Mefloquine 67-70 cyclin dependent kinase 5 regulatory subunit 1 Homo sapiens 177-181 22986170-10 2012 Finally, to elucidate whether the gap junction blocker mefloquine (MFQ) previously shown to dampen ACx SOs in slices affected GABAergic transmission, MFQ was acutely applied in P3-5 slices while spontaneous inhibitory postsynaptic currents (sIPSCs) were recorded. Mefloquine 150-153 cyclin dependent kinase 5 regulatory subunit 1 Homo sapiens 177-181 22972801-9 2012 Moreover, lipoapoptosis stimulated uptake of a membrane impermeable dye YoPro-1 (indicative of panx1 activation), which was inhibited by panx1 shRNA, probenecid, and mefloquine. Mefloquine 166-176 pannexin 1 Homo sapiens 95-100 22837476-4 2012 Mefloquine has been demonstrated to cause blockade of gap junction protein alpha 1 (GJA1) gap junction intercellular communication (GJIC), and recent evidence suggests that GJA1 GJIC is critical to successful embryonic implantation and early placental development. Mefloquine 0-10 gap junction protein alpha 1 Homo sapiens 54-82 22837476-4 2012 Mefloquine has been demonstrated to cause blockade of gap junction protein alpha 1 (GJA1) gap junction intercellular communication (GJIC), and recent evidence suggests that GJA1 GJIC is critical to successful embryonic implantation and early placental development. Mefloquine 0-10 gap junction protein alpha 1 Homo sapiens 84-88 22837476-5 2012 During routine use, mefloquine accumulates in organ and peripheral tissue, crosses the blood-placental barrier, and may plausibly accumulate in developing decidua and trophoblast at concentrations sufficient to interfere with GJA1 GJIC and, thus, cause deleterious effects on fetal outcomes. Mefloquine 20-30 gap junction protein alpha 1 Homo sapiens 226-230 22309769-4 2012 We found one specific mefloquine-binding protein that was identified by mass spectrometry as the glycolytic enzyme enolase (Q27877). Mefloquine 22-32 Enolase Escherichia coli 115-122 22309769-6 2012 In schistosomula crude extracts enolase activity was inhibited by mefloquine and by the enolase inhibitor sodium fluoride, while activity of the recombinant enolase was not affected. Mefloquine 66-76 Enolase Escherichia coli 32-39 21241737-6 2011 Furthermore, we have utilized a system biology-centered approach and have constructed a pathway model of cellular responses to mefloquine, identifying non-receptor tyrosine kinase 2 (Pyk2) as a critical target in mediating mefloquine neurotoxicity. Mefloquine 223-233 protein tyrosine kinase 2 beta Rattus norvegicus 183-187 21241737-8 2011 We have examined whether the downregulation of Pyk2 in primary rat cortical neurons alters mefloquine neurotoxicity by evaluating cell viability, apoptosis and oxidative stress. Mefloquine 91-101 protein tyrosine kinase 2 beta Rattus norvegicus 47-51 21241737-9 2011 Results from our study have confirmed that mefloquine neurotoxicity is associated with apoptotic response and oxidative injury, and we have demonstrated that mefloquine affects primary rat cortical neurons, at least in part, via Pyk2. Mefloquine 158-168 protein tyrosine kinase 2 beta Rattus norvegicus 229-233 21763755-4 2011 In area CA3, connexin 36 (Cx36) proteins are present and potentially sensitive to mefloquine. Mefloquine 82-92 carbonic anhydrase 3 Rattus norvegicus 8-11 21763755-4 2011 In area CA3, connexin 36 (Cx36) proteins are present and potentially sensitive to mefloquine. Mefloquine 82-92 gap junction protein, delta 2 Rattus norvegicus 13-24 21763755-4 2011 In area CA3, connexin 36 (Cx36) proteins are present and potentially sensitive to mefloquine. Mefloquine 82-92 gap junction protein, delta 2 Rattus norvegicus 26-30 21763755-5 2011 Here, we used hippocampal slices of adult rats to investigate the effects of mefloquine, which blocks Cx36, Cx43 and Cx50 gap junctions on both SPW-Rs and REDs. Mefloquine 77-87 gap junction protein, delta 2 Rattus norvegicus 102-106 21763755-5 2011 Here, we used hippocampal slices of adult rats to investigate the effects of mefloquine, which blocks Cx36, Cx43 and Cx50 gap junctions on both SPW-Rs and REDs. Mefloquine 77-87 gap junction protein, alpha 1 Rattus norvegicus 108-112 21763755-5 2011 Here, we used hippocampal slices of adult rats to investigate the effects of mefloquine, which blocks Cx36, Cx43 and Cx50 gap junctions on both SPW-Rs and REDs. Mefloquine 77-87 gap junction protein, alpha 8 Rattus norvegicus 117-121 21763755-10 2011 Intracellular recordings of CA3 pyramidal cells revealed that mefloquine did not change their resting membrane potential and input resistance but significantly increased the afterhyperpolarization following evoked action potentials (APs) resulting in reduced probability of AP firing during depolarizing current injection. Mefloquine 62-72 carbonic anhydrase 3 Rattus norvegicus 28-31 21764445-0 2011 Mefloquine blockade of connexin 43 (Cx43) and risk of pregnancy loss. Mefloquine 0-10 gap junction protein alpha 1 Homo sapiens 23-34 21764445-0 2011 Mefloquine blockade of connexin 43 (Cx43) and risk of pregnancy loss. Mefloquine 0-10 gap junction protein alpha 1 Homo sapiens 36-40 21638336-5 2011 Cx36 KO mice, and WT mice treated with the Cx36 antagonist mefloquine (MFQ), consumed significantly less ethanol than their WT controls in the drink-in-the-dark procedure. Mefloquine 71-74 gap junction protein, delta 2 Mus musculus 43-47 21302473-0 2010 [Polymorphism at the MDR1 locus as a cause of mefloquine-induced psychosis]. Mefloquine 46-56 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 20859773-8 2011 Mefloquine-treated utricles were positive for the extrinsic initiator caspase-8 and intrinsic initiator caspase-9 and downstream executioner caspase-3. Mefloquine 0-10 caspase 8 Rattus norvegicus 70-79 20859773-8 2011 Mefloquine-treated utricles were positive for the extrinsic initiator caspase-8 and intrinsic initiator caspase-9 and downstream executioner caspase-3. Mefloquine 0-10 caspase 9 Rattus norvegicus 104-113 20859773-8 2011 Mefloquine-treated utricles were positive for the extrinsic initiator caspase-8 and intrinsic initiator caspase-9 and downstream executioner caspase-3. Mefloquine 0-10 caspase 3 Rattus norvegicus 141-150 20859773-9 2011 These results indicate that mefloquine can induce significant hair cell degeneration in the postnatal rat utricle and that mefloquine-induced hair cell death is initiated by both caspase-8 and caspase-9. Mefloquine 123-133 caspase 8 Rattus norvegicus 179-188 20859773-9 2011 These results indicate that mefloquine can induce significant hair cell degeneration in the postnatal rat utricle and that mefloquine-induced hair cell death is initiated by both caspase-8 and caspase-9. Mefloquine 123-133 caspase 9 Rattus norvegicus 193-202 21267638-3 2011 Antagonists of both pannexin-1 (carbenoxolone and mefloquine) and P2X7 receptors (brilliant blue G) are known to block IPC when administered at the time of preconditioning (Vessey et al. Mefloquine 50-60 Pannexin 1 Rattus norvegicus 20-30 20932608-1 2010 In this work, we report the synthesis and the antitubercular evaluation of 16 new mefloquine derivatives, formed from reactions between mefloquine and benzaldehydes, with the activity expressed as the minimum inhibitory concentration (MIC) in muM. Mefloquine 82-92 latexin Homo sapiens 243-246 20943940-6 2010 However, the NMDAR-mediated neuronal death is prevented by pharmacological blockade of neuronal gap junctions (with mefloquine, 30 mg/kg) and does not occur in mice lacking neuronal gap junction protein, connexin 36. Mefloquine 116-126 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 13-18 21606109-4 2011 Unexpectedly, cells expressing Cx45, but not other Cxs, exhibited full coupling recovery after alkalization with NH4Cl under the continuous presence of LCCAs, isoflurane and mefloquine. Mefloquine 174-184 gap junction protein gamma 1 Homo sapiens 31-35 21502926-2 2011 Because mefloquine is a Cationic amphiphilic drug and is known to insert into lipid bilayers, we postulate that mefloquine interferes with the interaction between PIP2 and Kir channels resulting in channel inhibition. Mefloquine 8-18 killer cell immunoglobulin like receptor, two Ig domains and long cytoplasmic tail 4 Homo sapiens 172-175 21502926-2 2011 Because mefloquine is a Cationic amphiphilic drug and is known to insert into lipid bilayers, we postulate that mefloquine interferes with the interaction between PIP2 and Kir channels resulting in channel inhibition. Mefloquine 112-122 killer cell immunoglobulin like receptor, two Ig domains and long cytoplasmic tail 4 Homo sapiens 172-175 21502926-4 2011 The order of mefloquine inhibition was Kir6.2/SUR2A Kir2.3 (IC50 2 muM) > Kir2.1 (IC50 > 30 muM). Mefloquine 13-23 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 39-45 21502926-4 2011 The order of mefloquine inhibition was Kir6.2/SUR2A Kir2.3 (IC50 2 muM) > Kir2.1 (IC50 > 30 muM). Mefloquine 13-23 potassium inwardly rectifying channel subfamily J member 4 Homo sapiens 54-60 21502926-4 2011 The order of mefloquine inhibition was Kir6.2/SUR2A Kir2.3 (IC50 2 muM) > Kir2.1 (IC50 > 30 muM). Mefloquine 13-23 potassium inwardly rectifying channel subfamily J member 2 Homo sapiens 81-87 21502926-8 2011 Our results support the idea that mefloquine interferes with PIP2-Kir channels interactions. Mefloquine 34-44 killer cell immunoglobulin like receptor, two Ig domains and long cytoplasmic tail 4 Homo sapiens 66-69 21302473-5 2010 Genetic studies have found polymorphism at the MDR1 gene with genotypes 3435TT and 2677TT which underlie high levels of mefloquine in the brain. Mefloquine 120-130 ATP binding cassette subfamily B member 1 Homo sapiens 47-51 17352848-1 2007 The present report deals with the status of hepatic and splenic glutathione-S-transferase (GST) activities in mice during experimental infection with Plasmodium yoelii nigeriensis and subsequent treatment of infected mice with mefloquine (Mf) and menadione (Md). Mefloquine 227-237 hematopoietic prostaglandin D synthase Mus musculus 64-89 19656408-5 2009 This paper reviews the scientific evidence associating mefloquine with alterations in neuronal function, and it suggests the novel hypothesis that among those with the prevalent EPM1 mutation, inherited and mefloquine-induced impairments in neuronal physiologic safeguards might increase risk of GABAergic seizure during mefloquine chemoprophylaxis. Mefloquine 55-65 cystatin B Homo sapiens 178-182 19656408-5 2009 This paper reviews the scientific evidence associating mefloquine with alterations in neuronal function, and it suggests the novel hypothesis that among those with the prevalent EPM1 mutation, inherited and mefloquine-induced impairments in neuronal physiologic safeguards might increase risk of GABAergic seizure during mefloquine chemoprophylaxis. Mefloquine 207-217 cystatin B Homo sapiens 178-182 19656408-5 2009 This paper reviews the scientific evidence associating mefloquine with alterations in neuronal function, and it suggests the novel hypothesis that among those with the prevalent EPM1 mutation, inherited and mefloquine-induced impairments in neuronal physiologic safeguards might increase risk of GABAergic seizure during mefloquine chemoprophylaxis. Mefloquine 207-217 cystatin B Homo sapiens 178-182 19656408-6 2009 TESTING AND IMPLICATIONS OF THE HYPOTHESIS: Consistent with case reports of tonic-clonic seizures occurring during mefloquine chemoprophylaxis among those with family histories of epilepsy, it is proposed here that a new contraindication to mefloquine use be recognized for people with EPM1 mutation and for those with a personal history of myoclonus or ataxia, or a family history of degenerative neurologic disorder consistent with EPM1. Mefloquine 115-125 cystatin B Homo sapiens 286-290 19656408-6 2009 TESTING AND IMPLICATIONS OF THE HYPOTHESIS: Consistent with case reports of tonic-clonic seizures occurring during mefloquine chemoprophylaxis among those with family histories of epilepsy, it is proposed here that a new contraindication to mefloquine use be recognized for people with EPM1 mutation and for those with a personal history of myoclonus or ataxia, or a family history of degenerative neurologic disorder consistent with EPM1. Mefloquine 115-125 cystatin B Homo sapiens 434-438 18598190-4 2008 IPTp efficacy was assessed using data from an ongoing clinical trial to compare sulfadoxine-pyrimethamine with mefloquine that began in the same maternity clinics during July 2005; the present analysis is limited to women who delivered between November 2005 and November 2006. Mefloquine 111-121 tRNA isopentenyltransferase 1 Homo sapiens 0-4 18311193-4 2008 KEY RESULTS: 5-HT(3A) receptor responses were inhibited by mefloquine, quinine and chloroquine with IC(50) values of 0.66, 1.06 and 24.3 microM. Mefloquine 59-69 5-hydroxytryptamine receptor 3A Homo sapiens 13-20 18311193-6 2008 Mefloquine, quinine and chloroquine had higher IC(50) values at GABA(A) alpha1beta2 (98.7, 0.40 and 0.46 mM, respectively) and GABA(A) alpha1beta2gamma2 receptors (0.38, 1.69 and 0.67 mM, respectively). Mefloquine 0-10 adrenoceptor alpha 1D Homo sapiens 135-152 18311193-11 2008 CONCLUSIONS AND IMPLICATIONS: The effects of mefloquine, quinine and chloroquine are distinct at GABA(A) and GABA(C) receptors, whereas their effects on 5-HT(3AB) receptors are broadly similar to those at 5-HT(3A) receptors. Mefloquine 45-55 5-hydroxytryptamine receptor 3A Homo sapiens 153-160 20436212-8 2010 The quinoline agent mefloquine inhibited WT KCNQ1+KCNE1 with an IC(50) of 3.4 muM compared to 3.3 muM for V307L KCNQ1+KCNE1 (P >0.05). Mefloquine 20-30 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 44-49 20436212-8 2010 The quinoline agent mefloquine inhibited WT KCNQ1+KCNE1 with an IC(50) of 3.4 muM compared to 3.3 muM for V307L KCNQ1+KCNE1 (P >0.05). Mefloquine 20-30 potassium voltage-gated channel subfamily E regulatory subunit 1 Homo sapiens 50-55 20436212-8 2010 The quinoline agent mefloquine inhibited WT KCNQ1+KCNE1 with an IC(50) of 3.4 muM compared to 3.3 muM for V307L KCNQ1+KCNE1 (P >0.05). Mefloquine 20-30 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 112-117 20436212-8 2010 The quinoline agent mefloquine inhibited WT KCNQ1+KCNE1 with an IC(50) of 3.4 muM compared to 3.3 muM for V307L KCNQ1+KCNE1 (P >0.05). Mefloquine 20-30 potassium voltage-gated channel subfamily E regulatory subunit 1 Homo sapiens 118-123 20436212-9 2010 This establishes mefloquine as an effective inhibitor of recombinant "I(Ks)" channels incorporating this SQT2 KCNQ1 mutation. Mefloquine 17-27 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 105-109 20436212-9 2010 This establishes mefloquine as an effective inhibitor of recombinant "I(Ks)" channels incorporating this SQT2 KCNQ1 mutation. Mefloquine 17-27 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 110-115 20218915-0 2009 Mefloquine blockade of Pannexin1 currents: resolution of a conflict. Mefloquine 0-10 Pannexin 1 Rattus norvegicus 23-32 20218915-1 2009 The authors" laboratory has reported potent block of Pannexin1 (Panx1) currents by the antimalarial quinine derivative mefloquine. Mefloquine 119-129 Pannexin 1 Rattus norvegicus 53-62 20218915-1 2009 The authors" laboratory has reported potent block of Pannexin1 (Panx1) currents by the antimalarial quinine derivative mefloquine. Mefloquine 119-129 Pannexin 1 Rattus norvegicus 64-69 18973419-6 2008 Because many antimalarial agents are effluxed by P-gp (mefloquine, quinine), it was important to determine whether CF1 mice can develop cerebral malaria to predict drug toxicity during cerebral malaria. Mefloquine 55-65 phosphoglycolate phosphatase Mus musculus 49-53 18596211-4 2008 Activation of Panx1 currents following P2X(7)R stimulation or by membrane depolarization was blocked by Panx1 small-interfering RNA (siRNA) and with mefloquine > carbenoxolone > flufenamic acid. Mefloquine 149-159 pannexin 1 Homo sapiens 14-19 18596211-4 2008 Activation of Panx1 currents following P2X(7)R stimulation or by membrane depolarization was blocked by Panx1 small-interfering RNA (siRNA) and with mefloquine > carbenoxolone > flufenamic acid. Mefloquine 149-159 purinergic receptor P2X 7 Homo sapiens 39-46 17352848-1 2007 The present report deals with the status of hepatic and splenic glutathione-S-transferase (GST) activities in mice during experimental infection with Plasmodium yoelii nigeriensis and subsequent treatment of infected mice with mefloquine (Mf) and menadione (Md). Mefloquine 227-237 hematopoietic prostaglandin D synthase Mus musculus 91-94 17352848-1 2007 The present report deals with the status of hepatic and splenic glutathione-S-transferase (GST) activities in mice during experimental infection with Plasmodium yoelii nigeriensis and subsequent treatment of infected mice with mefloquine (Mf) and menadione (Md). Mefloquine 239-241 hematopoietic prostaglandin D synthase Mus musculus 91-94 17015054-0 2006 MDR1 gene polymorphisms are associated with neuropsychiatric adverse effects of mefloquine. Mefloquine 80-90 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 17015054-2 2006 We hypothesized that neuropsychiatric adverse effects of mefloquine are associated with polymorphisms in the MDR1/ABCB1 gene that encodes for the efflux pump P-glycoprotein. Mefloquine 57-67 ATP binding cassette subfamily B member 1 Homo sapiens 109-113 17015054-2 2006 We hypothesized that neuropsychiatric adverse effects of mefloquine are associated with polymorphisms in the MDR1/ABCB1 gene that encodes for the efflux pump P-glycoprotein. Mefloquine 57-67 ATP binding cassette subfamily B member 1 Homo sapiens 114-119 17015054-2 2006 We hypothesized that neuropsychiatric adverse effects of mefloquine are associated with polymorphisms in the MDR1/ABCB1 gene that encodes for the efflux pump P-glycoprotein. Mefloquine 57-67 ATP binding cassette subfamily B member 1 Homo sapiens 158-172 17015054-9 2006 CONCLUSION: In this study the MDR1 1236TT, 2677TT, and 3435TT genotypes, along with the 1236-2677-3435 TTT haplotype, were associated with neuropsychiatric adverse effects of mefloquine in women. Mefloquine 175-185 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 17015054-10 2006 MDR1 polymorphisms may play an important role in predicting the occurrence of neuropsychiatric adverse effects of mefloquine, particularly in female travelers. Mefloquine 114-124 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 16575850-5 2006 The Cx36 GJ blocker mefloquine (30 mg/kg) suppressed VTA GABA neuron ICPSDs in mature freely behaving rats. Mefloquine 20-30 gap junction protein, delta 2 Rattus norvegicus 4-8 16773639-6 2006 Mefloquine (50 mg/kg), which blocks gap junctions containing connexin 36, robustly suppressed harmaline tremor. Mefloquine 0-10 gap junction protein, delta 2 Mus musculus 61-72 16892398-0 2006 Design, synthesis, and SAR studies of mefloquine-based ligands as potential antituberculosis agents. Mefloquine 38-48 sarcosine dehydrogenase Homo sapiens 23-26 16772377-8 2006 Mefloquine, a close derivative of quinine and quinidine that exhibits antimalarial and antiarrhythmic properties, reduced conductance of cell-cell junctions and dye uptake through mCx30.2 hemichannels with approximately the same affinity (IC(50) = approximately 10 microM) and increased dependence of junctional conductance on transjunctional voltage. Mefloquine 0-10 gap junction protein, delta 3 Mus musculus 180-187 16843615-2 2006 PRESENTATION OF THE HYPOTHESIS: Psychosis is caused by interactions with other drugs or by pharmacogenetic vulnerabilities that cause heightened responses to chloroquine or mefloquine alone, mediated through dopamine, acetylcholine, serotonin, P-glycoprotein, inhibited cortical activity, deranged calcium homeostasis, and impaired synaptogenesis. Mefloquine 173-183 ATP binding cassette subfamily B member 1 Homo sapiens 244-258 16004972-0 2005 Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes. Mefloquine 16-26 ATP binding cassette subfamily C member 1 Homo sapiens 46-50 17091216-1 2006 Mefloquine (MFQ) selectively blocks exogenously expressed gap junction channels composed of Cx50 but not Cx46. Mefloquine 0-10 gap junction protein, alpha 8 Mus musculus 92-96 17091216-1 2006 Mefloquine (MFQ) selectively blocks exogenously expressed gap junction channels composed of Cx50 but not Cx46. Mefloquine 12-15 gap junction protein, alpha 8 Mus musculus 92-96 17091216-4 2006 When WT lenses were exposed to MFQ, the DF coupling conductance decreased significantly, suggesting that Cx50 contributes about 57% of the coupling conductance in DF and Cx46 contributes 43%. Mefloquine 31-34 gap junction protein, alpha 8 Mus musculus 105-109 17091216-4 2006 When WT lenses were exposed to MFQ, the DF coupling conductance decreased significantly, suggesting that Cx50 contributes about 57% of the coupling conductance in DF and Cx46 contributes 43%. Mefloquine 31-34 gap junction protein, alpha 3 Mus musculus 170-174 17091216-6 2006 Since MFQ is a selective blocker of Cx50 channels, it appears that Cx46 channels lack pH-mediated gating in the absence of functional Cx50 channels but are pH-sensitive in the presence of Cx50 channels. Mefloquine 6-9 gap junction protein, alpha 8 Mus musculus 36-40 17091216-6 2006 Since MFQ is a selective blocker of Cx50 channels, it appears that Cx46 channels lack pH-mediated gating in the absence of functional Cx50 channels but are pH-sensitive in the presence of Cx50 channels. Mefloquine 6-9 gap junction protein, alpha 3 Mus musculus 67-71 16081111-5 2005 Here, we demonstrate that mefloquine inhibits human recombinant acetylcholinesterase. Mefloquine 26-36 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-84 16081111-11 2005 Mefloquine also prolonged mepps at endplates of acetylcholinesterase knock-out mice. Mefloquine 0-10 acetylcholinesterase Mus musculus 48-68 16081111-12 2005 Since the selective butyrylcholinesterase inhibitor iso-OMPA (100 microM) also prolonged mepp decay at the neuromuscular junction of acetylcholinesterase knock-out mice, mefloquine inhibition of this enzyme is physiologically relevant. Mefloquine 170-180 acetylcholinesterase Mus musculus 133-153 16004972-0 2005 Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes. Mefloquine 16-26 ATP binding cassette subfamily C member 1 Homo sapiens 52-57 16004972-0 2005 Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes. Mefloquine 16-26 ATP binding cassette subfamily C member 4 Homo sapiens 63-67 16004972-0 2005 Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes. Mefloquine 16-26 ATP binding cassette subfamily C member 4 Homo sapiens 69-74 16004972-4 2005 Using inside-out vesicles prepared from human erythrocytes we have shown that mefloquine and MK-571 inhibit transport of 3 microM [(3)H]DNP-SG known to be mediated by MRP1 (IC(50) 127 and 1.1 microM, respectively) and of 3.3 microM [(3)H]cGMP thought but not proven to be mediated primarily by MRP4 (IC(50) 21 and 0.41 microM). Mefloquine 78-88 ATP binding cassette subfamily C member 1 Homo sapiens 167-171 16004972-4 2005 Using inside-out vesicles prepared from human erythrocytes we have shown that mefloquine and MK-571 inhibit transport of 3 microM [(3)H]DNP-SG known to be mediated by MRP1 (IC(50) 127 and 1.1 microM, respectively) and of 3.3 microM [(3)H]cGMP thought but not proven to be mediated primarily by MRP4 (IC(50) 21 and 0.41 microM). Mefloquine 78-88 ATP binding cassette subfamily C member 4 Homo sapiens 294-298 15596513-11 2005 The antimalarial drug mefloquine, which selectively blocks Cx50 and not Cx46 GJs, shows the same selectivity in Cx50 and Cx46 hemichannels indicating that the actions of such uncoupling agents, like voltage gating, are intrinsic hemichannel properties. Mefloquine 22-32 gap junction protein alpha 8 Homo sapiens 59-63 16004972-8 2005 These results demonstrate that mefloquine and MK-571 both inhibit transport of other substrates and stimulate ATPase activity and thus may themselves be substrates for transport. Mefloquine 31-41 dynein axonemal heavy chain 8 Homo sapiens 110-116 15896247-11 2005 One of possible mechanisms of the increase in plasma mefloquine concentrations may be the result of the inhibition of CYP3A4 by ketoconazole. Mefloquine 53-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 15596513-11 2005 The antimalarial drug mefloquine, which selectively blocks Cx50 and not Cx46 GJs, shows the same selectivity in Cx50 and Cx46 hemichannels indicating that the actions of such uncoupling agents, like voltage gating, are intrinsic hemichannel properties. Mefloquine 22-32 gap junction protein alpha 3 Homo sapiens 72-76 15596513-11 2005 The antimalarial drug mefloquine, which selectively blocks Cx50 and not Cx46 GJs, shows the same selectivity in Cx50 and Cx46 hemichannels indicating that the actions of such uncoupling agents, like voltage gating, are intrinsic hemichannel properties. Mefloquine 22-32 gap junction protein alpha 8 Homo sapiens 112-116 15596513-11 2005 The antimalarial drug mefloquine, which selectively blocks Cx50 and not Cx46 GJs, shows the same selectivity in Cx50 and Cx46 hemichannels indicating that the actions of such uncoupling agents, like voltage gating, are intrinsic hemichannel properties. Mefloquine 22-32 gap junction protein alpha 3 Homo sapiens 121-125 15328125-4 2004 Mefloquine plus moxifloxacin or mefloquine plus SRI-286 were better than mefloquine alone. Mefloquine 73-83 sorcin Mus musculus 48-51 14729380-7 2004 In conclusion, lumefantrine and desbutyl-lumefantrine inhibited significantly the hERG tail current with a higher IC50-value than mefloquine, chloroquine and halofantrine. Mefloquine 130-140 ETS transcription factor ERG Homo sapiens 82-86 15297615-0 2004 Potent block of Cx36 and Cx50 gap junction channels by mefloquine. Mefloquine 55-65 gap junction protein, delta 2 Mus musculus 16-20 15297615-0 2004 Potent block of Cx36 and Cx50 gap junction channels by mefloquine. Mefloquine 55-65 gap junction protein, alpha 8 Mus musculus 25-29 15297615-8 2004 Mefloquine also blocked channels formed by the lens gap junction protein, Cx50 (IC(50) approximately 1.1 microM). Mefloquine 0-10 gap junction protein, alpha 8 Mus musculus 74-78 15297615-14 2004 Thus, mefloquine is expected to be a useful tool to study the functional roles of Cx36 and Cx50. Mefloquine 6-16 gap junction protein, delta 2 Mus musculus 82-86 15297615-14 2004 Thus, mefloquine is expected to be a useful tool to study the functional roles of Cx36 and Cx50. Mefloquine 6-16 gap junction protein, alpha 8 Mus musculus 91-95 14663021-1 2003 During a program to investigate the biochemical basis of side effects associated with the antimalarial drug mefloquine, the authors made the unexpected discovery that the (-)-(R,S)-enantiomer of the drug is a potent adenosine A2A receptor antagonist. Mefloquine 108-118 adenosine A2a receptor Homo sapiens 216-238 12864851-9 2003 pfmdr1 transcript levels specifically increased 2.5-fold at 6 h in mefloquine-treated parasites and threefold in parasites treated with quinine for 30 min. Mefloquine 67-77 multidrug resistance protein 1 Plasmodium falciparum 3D7 0-6 12675948-10 2003 RESULTS: Based on RT-PCR, mefloquine upregulated cJun, IkappaB and GADD153. Mefloquine 26-36 DNA-damage inducible transcript 3 Rattus norvegicus 67-74 12848898-8 2003 The transcription of key ER proteins including GADD153, PERK, GRP78, PDI, GRP94 and calreticulin were up-regulated by mefloquine, suggesting that the drug induced an ER stress response. Mefloquine 118-128 DNA-damage inducible transcript 3 Rattus norvegicus 47-54 12848898-8 2003 The transcription of key ER proteins including GADD153, PERK, GRP78, PDI, GRP94 and calreticulin were up-regulated by mefloquine, suggesting that the drug induced an ER stress response. Mefloquine 118-128 heat shock protein family A (Hsp70) member 5 Rattus norvegicus 62-67 12848898-8 2003 The transcription of key ER proteins including GADD153, PERK, GRP78, PDI, GRP94 and calreticulin were up-regulated by mefloquine, suggesting that the drug induced an ER stress response. Mefloquine 118-128 prolyl 4-hydroxylase subunit beta Rattus norvegicus 69-72 12848898-8 2003 The transcription of key ER proteins including GADD153, PERK, GRP78, PDI, GRP94 and calreticulin were up-regulated by mefloquine, suggesting that the drug induced an ER stress response. Mefloquine 118-128 heat shock protein 90 beta family member 1 Rattus norvegicus 74-79 12848898-8 2003 The transcription of key ER proteins including GADD153, PERK, GRP78, PDI, GRP94 and calreticulin were up-regulated by mefloquine, suggesting that the drug induced an ER stress response. Mefloquine 118-128 calreticulin Rattus norvegicus 84-96 11897974-3 2002 The relation between the chirality of the drug mefloquine and the intracellular concentrations of the drug cyclosporine is illustrated by examining the effect of the enantiomers of mefloquine on the transport activity of P-glycoprotein (Pgp). Mefloquine 47-57 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 221-235 11897974-3 2002 The relation between the chirality of the drug mefloquine and the intracellular concentrations of the drug cyclosporine is illustrated by examining the effect of the enantiomers of mefloquine on the transport activity of P-glycoprotein (Pgp). Mefloquine 47-57 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 237-240 11897974-3 2002 The relation between the chirality of the drug mefloquine and the intracellular concentrations of the drug cyclosporine is illustrated by examining the effect of the enantiomers of mefloquine on the transport activity of P-glycoprotein (Pgp). Mefloquine 181-191 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 221-235 11897974-5 2002 The results demonstrated that (+)-mefloquine competitively displaced the Pgp substrate cyclosporine whereas (-)-mefloquine had no effect on cyclosporine-Pgp binding. Mefloquine 30-44 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 73-76 11732148-9 2001 These data support the use of combination therapy such as artesunate plus mefloquine for falciparum malaria in a hyperendemic area of Viet Nam. Mefloquine 74-84 SH3 and cysteine rich domain 3 Homo sapiens 139-142 8937469-0 1996 Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine. Mefloquine 81-91 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 11561091-0 2001 Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK and HERG. Mefloquine 38-48 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 91-97 11561091-0 2001 Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK and HERG. Mefloquine 38-48 potassium voltage-gated channel subfamily H member 2 Homo sapiens 107-111 11561091-3 2001 Mefloquine can prolong cardiac repolarization, especially when coadministered with halofantrine, an antagonist of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mefloquine 0-10 potassium voltage-gated channel subfamily H member 2 Homo sapiens 152-156 11561091-5 2001 Using patch-clamp electrophysiology we found that mefloquine inhibited KvLQT1/minK channel currents with an IC50 value of approximately 1 microM. Mefloquine 50-60 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 71-77 11561091-6 2001 Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones. Mefloquine 0-10 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 41-47 11561091-8 2001 HERG channel currents were about 6-fold less sensitive to block by mefloquine (IC50 = 5.6 microM). Mefloquine 67-77 potassium voltage-gated channel subfamily H member 2 Homo sapiens 0-4 11561091-10 2001 In contrast to structurally related drugs such as quinidine, mefloquine is a more effective antagonist of KvLQT1/minK compared with HERG. Mefloquine 61-71 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 106-112 11561091-11 2001 Block of KvLQT1/minK by mefloquine may involve an interaction with the closed state of the channel. Mefloquine 24-34 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 9-15 11561091-12 2001 Inhibition by mefloquine of KvLQT1/minK in the human heart may in part explain the synergistic prolongation of QT interval observed when this drug is coadministered with the HERG antagonist halofantrine. Mefloquine 14-24 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 28-34 11561091-12 2001 Inhibition by mefloquine of KvLQT1/minK in the human heart may in part explain the synergistic prolongation of QT interval observed when this drug is coadministered with the HERG antagonist halofantrine. Mefloquine 14-24 potassium voltage-gated channel subfamily H member 2 Homo sapiens 174-178 11683248-0 2001 The enantioselective binding of mefloquine enantiomers to P-glycoprotein determined using an immobilized P-glycoprotein liquid chromatographic stationary phase. Mefloquine 32-42 ATP binding cassette subfamily B member 1 Homo sapiens 58-72 11683248-0 2001 The enantioselective binding of mefloquine enantiomers to P-glycoprotein determined using an immobilized P-glycoprotein liquid chromatographic stationary phase. Mefloquine 32-42 ATP binding cassette subfamily B member 1 Homo sapiens 105-119 11031728-5 2000 Our results indicate that mefloquine inhibits the P-glycoprotein pump-efflux activity in a dose-related manner. Mefloquine 26-36 ATP binding cassette subfamily B member 1 Homo sapiens 50-64 11031728-6 2000 Moreover, mefloquine reduces the expression of the immunoreactive P-glycoprotein in K562/DXR cells as evaluated by cytofluorimetric assay. Mefloquine 10-20 ATP binding cassette subfamily B member 1 Homo sapiens 66-80 11031728-7 2000 Taken together, the results indicate that mefloquine reverses the multidrug-resistance phenotype through direct interaction with P-glycoprotein. Mefloquine 42-52 ATP binding cassette subfamily B member 1 Homo sapiens 129-143 9593122-5 1998 Cross-resistance assays determined that STI1 also conferred resistance to mefloquine (3.4-fold), while CIN5 also conferred resistance to mefloquine (9.6-fold) and chloroquine (5.4-fold). Mefloquine 74-84 Hsp90 cochaperone STI1 Saccharomyces cerevisiae S288C 40-44 9593122-5 1998 Cross-resistance assays determined that STI1 also conferred resistance to mefloquine (3.4-fold), while CIN5 also conferred resistance to mefloquine (9.6-fold) and chloroquine (5.4-fold). Mefloquine 137-147 Cin5p Saccharomyces cerevisiae S288C 103-107 9593122-6 1998 Using mefloquine as the selective drug, we determined that overexpression of YBR233w, a member of the hnRNPK family of nuclear RNA binding proteins, conferred resistance to mefloquine (13.5-fold). Mefloquine 6-16 heterogeneous nuclear ribonucleoprotein K Homo sapiens 102-108 9593122-6 1998 Using mefloquine as the selective drug, we determined that overexpression of YBR233w, a member of the hnRNPK family of nuclear RNA binding proteins, conferred resistance to mefloquine (13.5-fold). Mefloquine 173-183 heterogeneous nuclear ribonucleoprotein K Homo sapiens 102-108 9593122-7 1998 Expression of the human hnRNPK homolog of YBR233w in S. cerevisiae also conferred mefloquine resistance, suggesting that homologs of the identified resistance genes may perform similar functions in species other than yeast. Mefloquine 82-92 heterogeneous nuclear ribonucleoprotein K Homo sapiens 24-30 11113570-0 2000 Interactions of racemic mefloquine and its enantiomers with P-glycoprotein in an immortalised rat brain capillary endothelial cell line, GPNT. Mefloquine 24-34 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 60-74 11113570-3 2000 The interactions of racemic mefloquine and its individual enantiomers with the P-glycoprotein efflux transport system have been analysed in immortalised rat brain capillary endothelial GPNT cells. Mefloquine 28-38 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 79-93 11113570-5 2000 The cellular accumulation of the P-glycoprotein substrate, [(3)H]vinblastine, was significantly increased both in GPNT cells and in Caco-2 cells when treated with racemic mefloquine and the individual enantiomers. Mefloquine 171-181 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 33-47 11113570-7 2000 These results suggest that racemic mefloquine and its enantiomers are effective inhibitors of P-gp. Mefloquine 35-45 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 94-98 10831384-1 2000 A multidrug-resistant strain of Plasmodium yoelii nigeriensis (MDR) showing a wide spectrum of resistance to chloroquine, amodiaquine, mepacrine, mefloquine, halofantrine, quinine, and quinidine was used in this study for in vivo evaluation of the blood schizontocidal activity of pyronaridine, a topoisomerase II inhibitor, in Swiss mice. Mefloquine 146-156 malic enzyme complex, mitochondrial Mus musculus 63-66 8937469-0 1996 Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine. Mefloquine 81-91 ATP binding cassette subfamily B member 1 Homo sapiens 41-55 8937469-2 1996 Mefloquine, a quinolinemethanol antimalarial drug, was shown to inhibit the labelling of P-glycoprotein with an efficiency similar to that for verapamil, a known chemosensitizer. Mefloquine 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 89-103 8937469-4 1996 Mefloquine also inhibited the functional activity of P-glycoprotein. Mefloquine 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 53-67 8937469-6 1996 The ability of mefloquine to inhibit P-glycoprotein function may be involved in the neurotoxic side-effects occasionally associated with the use of mefloquine as an antimalarial drug. Mefloquine 15-25 ATP binding cassette subfamily B member 1 Homo sapiens 37-51 8937469-6 1996 The ability of mefloquine to inhibit P-glycoprotein function may be involved in the neurotoxic side-effects occasionally associated with the use of mefloquine as an antimalarial drug. Mefloquine 148-158 ATP binding cassette subfamily B member 1 Homo sapiens 37-51 7781845-8 1995 Rat islets of Langerhans exposed to mefloquine in vitro (10(-8) mol/l to 10(-3) mol/l) secreted significantly more insulin than control islets (up to 980 +/- 180 microU/ml/5 islets incubated with mefloquine 10(-3) mol/l, vs 20 +/- 4 microU/ml/5 untreated islets). Mefloquine 36-46 insulin Homo sapiens 115-122 2289299-2 1990 Mefloquine was administered alone (750 mg orally; group 1), or with primaquine (PQ, 45 mg; group 2), or in combination with sulfadoxine (1.5 g) + pyrimethamine (75 mg) (MSP; group 3), or as MSP + PQ (group 4). Mefloquine 0-10 macrophage stimulating 1 Homo sapiens 169-172 2385005-1 1990 The effects of the antimalarial agent mefloquine on the release of marker enzymes, acid phosphatase and beta glucuronidase, from the rat liver lysosomes in a crude lysosomal preparation were investigated and compared with that of chloroquine whose membrane effects have been well-documented in the literature. Mefloquine 38-48 glucuronidase, beta Rattus norvegicus 104-122 2289299-2 1990 Mefloquine was administered alone (750 mg orally; group 1), or with primaquine (PQ, 45 mg; group 2), or in combination with sulfadoxine (1.5 g) + pyrimethamine (75 mg) (MSP; group 3), or as MSP + PQ (group 4). Mefloquine 0-10 macrophage stimulating 1 Homo sapiens 190-193 34281730-0 2021 Corrigendum to "Mefloquine targets beta-catenin pathway and thus can play a role in the treatment of liver cancer" (Microb. Mefloquine 16-26 catenin beta 1 Homo sapiens 35-47 35417045-0 2022 Mefloquine induces ER stress and apoptosis in BRAFi-resistant A375-BRAFV600E /NRASQ61K malignant melanoma cells targeting intracranial tumors in a bioluminescent murine model. Mefloquine 0-10 neuroblastoma ras oncogene Mus musculus 78-82 2842264-2 1988 Mefloquine was found to significantly stimulate the release of lysozyme, beta-glucuronidase and myeloperoxide at a concentration of 10 micrograms/ml (2.5 X 10(-5) M) without loss of cell viability. Mefloquine 0-10 glucuronidase beta Homo sapiens 73-91 2842264-4 1988 Mefloquine at 10 micrograms/ml also significantly increased the release of lysozyme and beta-glucuronidase but not myeloperoxidase when neutrophils were stimulated with opsonized zymosan. Mefloquine 0-10 glucuronidase beta Homo sapiens 88-106